Hamdi Mohamed, Elmowafy Enas, Abdel-Bar Hend Mohamed, ElKashlan Akram M, Al-Jamal Khuloud T, Awad Gehanne A S
Department of Pharmaceutics, Faculty of Pharmacy, University of Sadat City, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Egypt.
Int J Biol Macromol. 2022 Sep 30;217:731-747. doi: 10.1016/j.ijbiomac.2022.07.067. Epub 2022 Jul 13.
Drug covalently bound to polymers had formed, lately, platforms with great promise in drug delivery. These drug polymer conjugates (DPC) boosted drug loading and controlled medicine release with targeting ability. Herein, the ability of entecavir (E) conjugated to hyaluronic acid (HA) forming the core of vitamin E coated lipid nanohybrids (EE-HA LPH), to target Kupffer cells and hepatocyte had been proved. The drug was associated to HA with efficiency of 93.48 ± 3.14 % and nanohybrids loading of 22.02 ± 2.3 %. DiI labelled lipidic nanohybrids improved the macrophage uptake in J774 cells with a 21 day hepatocytes retention post intramuscular injection. Finally, in vivo biocompatibility and safety with respect to body weight, organs indices and histopathological alterations were demonstrated. Coating with vitamin E and conjugation of E to HA (a CD44 ligand), could give grounds for prospective application for vectored nano-platform in hepatitis B.
药物与聚合物共价结合，近来已形成了在药物递送方面极具前景的平台。这些药物聚合物偶联物（DPC）提高了药物负载量，并具有靶向能力以控制药物释放。在此，已证明恩替卡韦（E）与透明质酸（HA）偶联形成维生素E包被的脂质纳米杂化物（EE-HA LPH）的核心，能够靶向库普弗细胞和肝细胞。药物与HA的结合效率为93.48±3.14%，纳米杂化物的负载率为22.02±2.3%。DiI标记的脂质纳米杂化物提高了J774细胞中巨噬细胞的摄取，肌肉注射后在肝细胞中保留21天。最后，证明了其在体重、器官指数和组织病理学改变方面的体内生物相容性和安全性。用维生素E包被以及将E与HA（一种CD44配体）偶联，可为乙肝病毒载体纳米平台的前瞻性应用提供依据。
